93735-22-9Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
-
Page/Page column 31; 32, (2021/06/11)
The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I, and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to
Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds
-
, (2009/01/20)
[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
Perry, Benjamin,Alexander, Rikki,Bennett, Gavin,Buckley, George,Ceska, Tom,Crabbe, Tom,Dale, Verity,Gowers, Lewis,Horsley, Helen,James, Lynwen,Jenkins, Kerry,Crepy, Karen,Kulisa, Claire,Lightfoot, Helen,Lock, Chris,Mack, Stephen,Morgan, Trevor,Nicolas, Anne-Lise,Pitt, Will,Sabin, Verity,Wright, Sara
scheme or table, p. 4700 - 4704 (2009/04/08)
The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
Production Method of Nitrogen-Containing Fused Ring Compounds
-
Page/Page column 50, (2010/11/30)
[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.
Nitrogen-containing fused ring compounds and use thereof
-
Page/Page column 86, (2010/11/25)
A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.
Synthesis of oxypropanolamine derivatives of 3,4-dihydro-2H-1,4- benzoxazine, β-adrenergic affinity, inotropic, chronotropic and coronary vasodilating activities
Iakovou, Kriton,Kazanis, Michalis,Vavayannis, Andreas,Bruni, Giancarlo,Romeo, Maria Raffaella,Massarelli, Paola,Teramoto, Shuji,Fujiki, Hiroyuki,Mori, Toyoki
, p. 903 - 917 (2007/10/03)
A series of oxypropanolamine derivatives of 3,4-dihydro-2H-1,4- benzoxazine were synthesized and evaluated for inotropic, chronotropic and coronary vasodilating activities in the canine heart, affinity to β1- adrenergic receptor in turkey erythrocytes and affinity to the β2- adrenergic receptor in the rat lung. Among these compounds, 4-acetyl-6-(3- tert-butylamino-2-hydroxy)propoxy-3,4-dihydro-2H-1,4-benzoxazine showed 2.1- fold more potent affinity to the β1 receptor than propranolol and 7-(3- tert-butylamino-2-hydroxy)propoxy-N-butyryl-3,4-dihydro-2H-1,4-benzoxazine showed 2.5-fold more potent affinity to the β2 receptor and furthermore 4 386-fold more potent selectivity to the β2 receptor than propranolol. In addition, 4-acetyl-6-[3-(3,4-dimethoxybenzyl)amino-2-hydroxy]propoxy-3,4- dihydro-2H-1,4-benzoxazine showed 1.1-fold more potent affinity to the β1 receptor than propranolol and also 1 147-fold more potent selectivity to the β1 receptor. With a few exceptions, negative inotropic and chronotropic actions of these compounds were dependent on the size of the 4-substituent obeying the order: unsubstituted 1-adrenoceptor nor coronary vasodilator action related with affinity to β2-adrenoceptor were observed. 4-acetyl-7- [3-(3,4-dimethoxybenzyl)amino-2-hydroxy]propoxy-3,4-dihydro-2H-1,4- benzoxazine exerted potent positive inotropic, chronotropic and coronary vasodilating actions. The inotropic and chronotropic actions of the latter compound may be attributed to the release of intrinsic catecholamines, as concluded by the absence of β1-adrenoceptor affinity and disappearance of activity in the presence of a β-blocker.
Cationic dyes
-
, (2008/06/13)
There are described novel greenish-yellow cationic dyes of the formula STR1 wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or NO2, R2 is unsubstituted lower alkyl, or lower alkyl which is substituted by: hydroxyl, lower alkoxy, halogen, CN, carboxylic acid amide, carboxylic acid alkyl ester or phenyl, or R2 is alkenyl (C3 -C4), the R3 's independently of one another are each lower alkyl, or both R3 's together form a carbocyclic 5-, 6- or 7-membered ring, R4 is hydrogen, lower alkyl, unsubstituted aryl or substituted aryl, R5, R6 and R7 independently of one another are hydrogen, lower alkyl, lower alkoxy, halogen, NO2, CN or lower alkylsulfonyl, and A is an anion; processes for producing them, and their use for dyeing and printing textile materials, particularly polyacrylonitrile materials.
